“…A solution of 4 [11] (2.60 g, 10.0 mmol) in MeOH (70 mL) was treated with succinic anhydride (1.20 g, 12.0 mmol, 1.2 eq) and stirred at room temperature until the starting material was completely disappeared (TLC, 9:1 EtOAc-i PrOH). After 2 h, Et 3 N (3 mL) was added to the reaction mixture, which was stirred for 10 min at room temperature and then was repeatedly coevaporated with toluene ( (7). A solution of amine 5 [8] (1.00 g, 1.97 mmol) and succinic anhydride (216 mg, 2.16 mmol, 1.2 eq) in MeOH (40 mL) was allowed to react in the reaction conditions described for the preparation of 6, leading to the residue (1.17 g) constituted exclusively ( 13 C NMR) by 7 (98% yield).…”